Drug Formulations Oral Formulations: Tablet, Capsule, Solution, Suspension, etc. Parenterals: Injections, Ophthalmics Inhalations Topicals

Dosage Forms Containing Solid API Tablet Capsule Ointment Suppository Suspension Oral Injection Inhalation Ophthalmic

Tablet Disintegration Dissolution Absorption

Particle Size Crystal Form Dissolution Tableting Properties Physical and Chemical Stability Solubility Important Solid-State Properties

Problems in Dosage forms Resulting from Use of the Wrong Polymorph Suspension (Aqueous vehicle) - Crystal growth leading to undesirableparticle size distribution, particularly, in parenteral suspensions, or caking Cream - Crystal growth, yielding gritty, cosmetically unacceptable creams ore uneven distribution of active ingredient Solution - Precipitation due to crystal growth Suppositories - Melting point changes of vehicles resulting in softening of product or hindrance in release of active ingredient

Chemical Stability Summary of the reactives of the α, β and γcrystalline forms of ethoxycinnamic acid exposure to ultraviolet light

Bioavailability Comparison of mean blood serum levels obtained with choramphenical palmitate suspension containing varying ratios of A and B polymorphs (per cent of Form B in the suspension: M, 0%; N 25%; O, 50%, P; 75%; L, 100%)

Tablet Friability: 30 tabs, wt loss < 1% Disintegration Dissolution Rate or Dissolution Profile Uniformity of Dosage Unit Weight Variation: 10 units Content Uniformity: 10 units Quality Control of Tablets

Tablet Formulation Filler: Starch, Lactose, Mannitol Microcrystalline Cellulose (Avecil) Binder: Starch, Acacia, Gelatin, Simple Syrup Lubricant: Mg Stearate, Ca Stearate, Talc Disintegrant: Starch, Avecil Flavor Colorant: D&C Misc. : Stabilizer

Pediatric Chewable Aspirin Tablet (wet granulation) Aspirin Mannitol Saccharin sodium Acacia Starch Stearic acid Talc Dry Flavor mg/tab

Tablet Manufacturing (Wet Granulation) Binder Preparation (10% Acacia) Sieving (Mannitol & Saccharin sodium) Mixing & Granulation Sieving (Aspirin, starch, Stearic acid, Talc, dry flavor) Mixing Drying Compression

Sustained Release Tablets Therapeutic Range Minimum Effective Level Time Toxic level Drug Concentration (units mL-1) “Ideal” sustained blood or tissue drug level versus time profile

Toxic level Minimum Effective Level Drug Concentration (units mL-1) Time Repetitive release approach to sustained-release.

Pores produces by soluble portion of polymer membrane Membrane Reservoir Mechanism of Sustained Release : Diffusion Diffusion control of drug release by a water-insoluble polymer (left) Diffusion control of drug release by a Partially water-soluble polymer (right)

Mechanism of Sustained release: Dissolution

Mechanism of Sustained Release : Osmosis